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光学活性化合物的合成可以追朔到上世纪中叶巴士德的传奇性研究。他不仅第一个认识到光学活性是由于分子具有不能重叠的镜像结构所产生的不对称性而引起的,而且他还开发了现仍被用于外消旋体工业化分离的两种重要方法。近年来,由于不断认识到光学纯度对生物活性的重要性,从而大大促进了人们对合成纯对映体的兴趣。譬如,有许多药物是手性分子,具有二个光学异构体,从生物活性的观点来看,这二个光学异构体应被视为是两种不同的物质。一般来说,外消旋混合物中仅仅只有一个对映体显示所希望的生物活性,大多数其它异构体就成了并不需要的压载物(ballast),甚至还能抑制有效的作用或显示不良的副作用。当认识到生物活性通常是由于药物与受
The synthesis of optically active compounds can be traced back to the legendary study of Bastian in the mid-last century. Not only did he first recognize that optical activity is due to the asymmetry created by the non-overlapping mirror structures of molecules, he also developed two important methods that are still being used for the industrial resolution of racemates. In recent years, interest in the synthesis of pure enantiomers has been greatly enhanced by the constant recognition of the importance of optical purity to biological activity. For example, many drugs are chiral molecules with two optical isomers, and from the biological activity point of view, these two optical isomers should be considered as two different substances. In general, only one enantiomer in a racemic mixture shows the desired biological activity, and most other isomers are unwanted ballast and even inhibit effective action or Shows bad side effects. When it comes to biological activity is usually due to the drug and subject